产品
编 号:F022192
分子式:C26H17N3Na2O8S2
分子量:609.54
产品类型
结构图
CAS No: 1052087-90-7
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产品详情
生物活性:
PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. The P2Y12 receptor plays a crucial role in platelet aggregation. Antithrombotic effect.
体内研究:
PSB-0739 (0.01-0.3 mg/kg, intrathecally) has dose-dependent and significant antihyperalgesic effect in low doses. The minimal effective dose (mED) is 0.1 mg/kg.Animal Model:Male Wistar rats, 150-250 g, 6-8/group
Dosage:0.01, 0.03, 0.1, 0.3 mg/kg
Administration:Intrathecal injection ( i.t.)
Result:Displayed a dose-dependent inhibitory effect on mechanical hyperalgesia in the range of 0.01–0.1 mg/kg.
体外研究:
PSB-0739 is a potent competitive non-nucleotide antagonist at the human P2Y12 receptor with a pA2 value of 9.8. PSB-0739 inhibits ADP-evoked Ca2+ responses with an EC50 of 5.4±1.8 μM and causes a rightward parallel shift in the ADP concentration–response curve in THP-1 cells.